[1H-Pyrazolo[3, 4-D]Pyrimidin-4-Yl]-Piperidine or -Piperazine Compounds as Serine-Theoronine Kinase Modulators (P70s6k, Atk1 and Atk2) for the Treatment of Immunological, Inflammatory and Proliferative Diseases
申请人:Rice Ken
公开号:US20080188482A1
公开(公告)日:2008-08-07
The invention provides compounds of formula (I) and methods for inhibition of kinases, more specifically p70S6 kinases, and more preferably p70S6, Akt-1 and Akt-2 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.
[EN] UII-MODULATING COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS MODULANT U II ET LEUR UTILISATION
申请人:ACADIA PHARM INC
公开号:WO2008057543A2
公开(公告)日:2008-05-15
[EN] Disclosed herein are novel aromatic-containing compounds and methods for using various aromatic-containing compounds for treatment and prevention of diseases and disorders related to the Urotensin II receptor. [FR] La présente invention concerne de nouveaux composés contenant un groupe aromatique et des procédés permettant d'utiliser divers composés contenant un groupe aromatique pour le traitement et la prévention de maladies et de troubles associés au récepteur de l'urotensine II.
Novel and potent small-molecule urotensin II receptor agonists
作者:Fredrik Lehmann、Erika A. Currier、Bryan Clemons、Lars K. Hansen、Roger Olsson、Uli Hacksell、Kristina Luthman
DOI:10.1016/j.bmc.2009.04.062
日期:2009.7
A series of analogs of the non-peptidic urotensin II receptor agonist N-[1-(4-chlorophenyl)-3-(dimethylamino)propyl]-4-phenylbenzamide (FL104) has been synthesized and evaluated pharmacologically. The enantiomers of the two most potent racemic analogues were obtained from the corresponding diastereomeric mandelic amides. In agreement with previously observed SAR, most of the agonist potency resided